盐酸依匹斯汀的合成工艺研究  

Synthesis technology of epinastine hydrochloride

作　　者：郭建锋[1] 张彩霞[1] 王彦丽[1] 孙歆慧[1] 郭振华[1] 

机构地区：[1]天津药物研究院,天津300193

出　　处：《现代药物与临床》2011年第5期378-380,共3页Drugs & Clinic

摘　　要：目的研究盐酸依匹斯汀的合成工艺。方法以6一氰基一6，11-1H-Z-苯并[b，e]氮杂革为起始原料，经硼氢化钠还原，富马酸盐精制，溴化氰环合得依匹斯汀溴酸盐，用氢氧化钠将其游离，再在乙醇中用盐酸成盐，用乙醇和水重结晶得盐酸依匹斯汀。结果所得的盐酸依匹斯汀的结构经’H—NMR、MS、IR等确证，总收率为55％，HPLC测定质量分数为99．96％。结论本合成工艺稳定，条件温和，操作简便，适合盐酸依匹斯汀的工业化生产。Objective To study the synthesis technology ofepinastine hydrochloride. Methods Using llH-dibenzo[b,e]azepine-6- carbonitrile as starting material, epinastine hydrochloride bromate was synthesized by reduction with sodium borohydride, refining with fumaric acid, cyclocondensation by cyanogen bromide. NaOH was used to liberate epinastine hydrochloride bromate and salification was done with HC1 in ethanol. And then epinastine hydrochloride was obtained through recrystallisation with ethanol and water. Results The structure of epinastine hydrochloride was confirmed by 1H-NMR, MS, IR, etc, and total yield was 55% with HPLC purity of 99.96%. Conclusion The synthesis technology of epinastine hydrochloride is stable, simple, high productive, and can be applied to industry production.

关 键 词：盐酸依匹斯汀 还原 环合 成盐 工业化 

分 类 号：R914.2[医药卫生—药物化学]